JH-VIII-157-02

Name: JH-VIII-157-02
Brand: MedChemExpress
SKU: HY-112140
Rating: 4.5 (1 reviews)

Cat. No.: HY-112140 Purity: 99.67%: FAQs
Data Sheet SDS COA Handling Instructions

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JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC₅₀ of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.

For research use only. We do not sell to patients.

JH-VIII-157-02 Chemical Structure

CAS No. : 1639422-97-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 430	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 430	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 630	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 980	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1820	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & Target

IC50: 2 nM (EML4-ALK G1202R, cell assay), 2 nM (EML4-ALK^wt, cell assay), 2 nM (EML4-ALK C1156Y, cell assay), 2 nM (EML4-ALK F1174L, cell assay), 2 nM (EML4-ALK F1174L, cell assay)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	107 nM Compound: 6; JH-VIII-157-02	Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	196 nM Compound: 6; JH-VIII-157-02	Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 nM Compound: 6; JH-VIII-157-02	Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 nM Compound: 6; JH-VIII-157-02	Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 nM Compound: 6; JH-VIII-157-02	Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 nM Compound: 6; JH-VIII-157-02	Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	2 nM Compound: 6; JH-VIII-157-02	Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	3 nM Compound: 6; JH-VIII-157-02	Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	58 nM Compound: 6; JH-VIII-157-02	Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
BaF3	IC₅₀	591 nM Compound: 6; JH-VIII-157-02	Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay	[PMID: 26568289]
Kelly	EC₅₀	147 nM Compound: 6; JH-VIII-157-02	Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
NCI-H3122	EC₅₀	5 nM Compound: 6; JH-VIII-157-02	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
NCI-H3122	IC₅₀	5.9 nM Compound: 21a	Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs	[PMID: 26476749]
SH-SY5Y	EC₅₀	413 nM Compound: 6; JH-VIII-157-02	Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-AS	EC₅₀	775 nM Compound: 6; JH-VIII-157-02	Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-FI	EC₅₀	973 nM Compound: 6; JH-VIII-157-02	Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]
SK-N-SH	EC₅₀	245 nM Compound: 6; JH-VIII-157-02	Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 26568289]

In Vitro

JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC₅₀ of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells. JH-VIII-157-02 also potently inhibits EML4-ALK^wt (Eawt), EAC1156Y, EAF1174L, EAS1206Y (IC₅₀, 2 nM), EAG1269A (IC₅₀, 3 nM), EAL1196M (IC₅₀, 58 nM), EA1151Tins (IC₅₀, 107 nM), and EAL1152R (IC₅₀, 196 nM). Moreover, JH-VIII-157-02 has selectivity at other kinases, including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4, and the IC₅₀s are 14 nM, 14 nM, 3 nM, 13 nM, 12 nM, and 465 nM respectively. JH-VIII-157-02 exhibits inhibitory growth of cancer cell lines, such as H3122, DFCI76 (L1152R] with EC₅₀s of 5, 19 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JH-VIII-157-02 exhibits good oral bioavailability following an oral dose of 10 mg/kg in mice. JH-VIII-157-02 also penetrates the CNS of mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

465.55

Formula

C₂₈H₂₇N₅O₂

CAS No.

1639422-97-1

Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C)C)CN1N=CC(C2=C(CC)C=C3C(C(C)(C)C(NC4=C5C=CC(C#N)=C4)=C5C3=O)=C2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 25 mg/mL (53.70 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1480 mL	10.7400 mL	21.4800 mL
5 mM	0.4296 mL	2.1480 mL	4.2960 mL
10 mM	0.2148 mL	1.0740 mL	2.1480 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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Purity & Documentation

Purity: 99.67%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (248 KB) LCMS (109 KB)

Handling Instructions (2659 KB)

References

[1]. Hatcher JM, et al. Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. J Med Chem. 2015 Dec 10;58(23):9296-9308. [Content Brief]

Cell Assay
^[1]

Cells are seeded at 4000 per well in 96 well plates and exposed to JH-VIII-157-02 in triplicate at 1 nM to 10 μM for 72 hours. Cell viability is evaluated using CellTiter-Glo Luminescent Cell Viability Assay. IC₅₀ values are calculated by nonlinear regression (variable slope) using GraphPad Prism 5 software. Each experiment is repeated for at least twice^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Hatcher JM, et al. Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. J Med Chem. 2015 Dec 10;58(23):9296-9308. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1480 mL	10.7400 mL	21.4800 mL	53.6999 mL
	5 mM	0.4296 mL	2.1480 mL	4.2960 mL	10.7400 mL
	10 mM	0.2148 mL	1.0740 mL	2.1480 mL	5.3700 mL
	15 mM	0.1432 mL	0.7160 mL	1.4320 mL	3.5800 mL
	20 mM	0.1074 mL	0.5370 mL	1.0740 mL	2.6850 mL
	25 mM	0.0859 mL	0.4296 mL	0.8592 mL	2.1480 mL
	30 mM	0.0716 mL	0.3580 mL	0.7160 mL	1.7900 mL
	40 mM	0.0537 mL	0.2685 mL	0.5370 mL	1.3425 mL
	50 mM	0.0430 mL	0.2148 mL	0.4296 mL	1.0740 mL

JH-VIII-157-02 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JH-VIII-157-021639422-97-1Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

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JH-VIII-157-02

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